104931-56-8
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- CAS号:
- 104931-56-8
- 英文名:
- Tranilast (SodiuM)
- 英文别名:
- Tranilast (SodiuM);Sodium 2-(3-(3,4-dimethoxyphenyl)acrylamido)benzoate
- 中文名:
- 104931-56-8
- 中文别名:
- 曲尼司特钠;化合物 T23472;2-(3-(3,4-二甲氧基苯基)丙烯酰胺基)苯甲酸钠
- CBNumber:
- CB32682023
- 分子式:
- C18H16NNaO5
- 分子量:
- 349.31311
- MOL File:
- 104931-56-8.mol
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104931-56-8化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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104931-56-8性质、用途与生产工艺
Tranilast sodium (MK-341 sodium) 是一种抗变态反应剂。抑制前列腺素 D2 产生 (PGD2，IC50=0.1 mM)。具有抗炎和免疫调节作用。Tranilast sodium 拮抗血管紧张素 II (angiotensin II) 并抑制其在血管平滑肌细胞中的生物学作用。
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PGD
2
0.1 mM (IC
50
)
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Angiotensin II
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Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC
50
=~1-20 μM), thromboxane B2 (IC
50
=~10-50 μM), (TGF-β1; IC
50
=~100-200 μM), and IL-8 (IC
50
=~100 μM) formation. A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC
50
s of 10-40 μM and 2-20 μM, respectively.
Tranilast (10-200 μM) exhibits the anti-proliferative effect in a dose-dependent manner in both MCF-7 and MDA-MB-231 cell lines. Tranilast also (10-200μM) enhances the anti-tumor effects of Tamoxifen (1-20 μM) on human breast cancer cells in vitro.
Tranilast (12.5, 25, 50, 100 μg/mL; 72 hours) inhibits proliferation of HDMECs.
Cell Proliferation Assay
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Cell Line:
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MCF-7 and MDA-MB-231 cells
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Concentration:
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10, 20, 50, 100, and 200 μM
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Incubation Time:
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48 hours
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Result:
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Anti-proliferative effect in a dose-dependent manner in both cell lines.
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Cell Proliferation Assay
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Cell Line:
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Human dermal microvascular endothelial cells (HDMECs)
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Concentration:
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12.5, 25, 50, 100 μg/mL
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Incubation Time:
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72 hours
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Result:
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IC
50
value was 44.3 μg/mL (136 μM).
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Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice.
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Animal Model:
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Nine-week-old male C57BL/6 mice
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Dosage:
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300 mg/kg
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Administration:
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Administered orally twice a day for 3 days
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Result:
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Suppressed the VEGF-induced angiogenesis in matrigel; 58% of significant suppression was observed at a dose of 300 mg/kg.
The ED
50
value and 95% confidence limits were 165 mg/kg and 162±169 mg/kg, respectively.
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104931-56-8
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104931-56-8, 104931-56-8 相关搜索:
- 2-(3-(3,4-二甲氧基苯基)丙烯酰胺基)苯甲酸钠
- 化合物 T23472
- 曲尼司特钠
- 104931-56-8
- Sodium 2-(3-(3,4-dimethoxyphenyl)acrylamido)benzoate
- Tranilast (SodiuM)